Literature DB >> 18752947

New PPARgamma ligands based on barbituric acid: virtual screening, synthesis and receptor binding studies.

Sandeep Sundriyal1, Bhoomi Viswanad, Poduri Ramarao, Asit K Chakraborti, Prasad V Bharatam.   

Abstract

A new series of PPARgamma ligands based on barbituric acid (BA) has been designed employing virtual screening and molecular docking approach. To validate the computational approach, designed molecules were synthesized and evaluated in in vitro radioligand binding studies. Out of the total 14 molecules, 6 were found to bind to the murine PPARgamma with IC(50) ranging from 0.1 to 2.5 microM as compared to reference standard, pioglitazone (IC(50)=0.7 microM).

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Year:  2008        PMID: 18752947     DOI: 10.1016/j.bmcl.2008.08.028

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

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Journal:  J Am Chem Soc       Date:  2017-05-10       Impact factor: 15.419

2.  Thiazolidinedione Derivatives: In Silico, In Vitro, In Vivo, Antioxidant and Anti-Diabetic Evaluation.

Authors:  Manal Y Sameeh; Manal M Khowdiary; Hisham S Nassar; Mahmoud M Abdelall; Hamada H Amer; Abdelaaty Hamed; Ahmed A Elhenawy
Journal:  Molecules       Date:  2022-01-27       Impact factor: 4.411

Review 3.  Understanding nuclear receptors using computational methods.

Authors:  Ni Ai; Matthew D Krasowski; William J Welsh; Sean Ekins
Journal:  Drug Discov Today       Date:  2009-03-11       Impact factor: 7.851

4.  Identification of small molecules that inhibit the histone chaperone Asf1 and its chromatin function.

Authors:  Ja-Hwan Seol; Tae-Yang Song; Se Eun Oh; Chanhee Jo; Ahreum Choi; Byungho Kim; Jinyoung Park; Suji Hong; Ilrang Song; Kwan Young Jung; Jae-Hyun Yang; Hwangseo Park; Jin-Hyun Ahn; Jeung-Whan Han; Eun-Jung Cho
Journal:  BMB Rep       Date:  2015-12       Impact factor: 4.778

5.  Structural Basis for the Enhanced Anti-Diabetic Efficacy of Lobeglitazone on PPARγ.

Authors:  Jun Young Jang; Hwan Bae; Yong Jae Lee; Young Il Choi; Hyun-Jung Kim; Seung Bum Park; Se Won Suh; Sang Wan Kim; Byung Woo Han
Journal:  Sci Rep       Date:  2018-01-08       Impact factor: 4.379

6.  Ovicidal and Insecticidal Activities of Pyriproxyfen Derivatives with an Oxime Ester Group.

Authors:  Guo-Shao Sun; Xin Xu; Shu-Hui Jin; Le Lin; Jian-Jun Zhang
Journal:  Molecules       Date:  2017-06-08       Impact factor: 4.411

7.  Use of a molecular beacon based fluorescent method for assaying uracil DNA glycosylase (Ung) activity and inhibitor screening.

Authors:  Avani Mehta; Prateek Raj; Sandeep Sundriyal; Balasubramanian Gopal; Umesh Varshney
Journal:  Biochem Biophys Rep       Date:  2021-02-15
  7 in total

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